+ Site Statistics
References:
54,258,434
Abstracts:
29,560,870
PMIDs:
28,072,757
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis



Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis



Bioorganic and Medicinal Chemistry Letters 21(3): 1015-1018



A series of compounds containing 2-substituted imidazoles has been synthesized from imidazole and tested for its biological activity against human African trypanosomiasis (HAT). The 2-substituted 5-nitroimidazoles such as fexinidazole (7a) and 1-[4-(1-methyl-5-nitro-1H-imidazol-2-ylmethoxy)-pyridin-2-yl-piperazine (9e) exhibited potent activity against T. brucei in vitro with low cytotoxicity and good solubility. The presence of the NO(2) group at the 5-position of the imidazole ring in 2-substituted imidazoles is the crucial factor to inhibit T. brucei.

Please choose payment method:






(PDF emailed within 0-6 h: $19.90)

Accession: 052269401

Download citation: RISBibTeXText

PMID: 21211967

DOI: 10.1016/j.bmcl.2010.12.040


Related references

Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms. Official Gazette of the United States Patent & Trademark Office Patents 1245(1), Apr 3, 2001

Evaluation of cryptolepine and huperzine derivatives as lead compounds towards new agents for the treatment of human African trypanosomiasis. Natural Product Communications 4(2): 193-198, 2009

Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis. Journal of Medicinal Chemistry 57(3): 828-835, 2014

Pathology of human African trypanosomiasis with reference to experimental African trypanosomiasis and infections of the central nervous system. British Medical Bulletin 41(2): 169-174, 1985

Report on a meeting of the product development team for African trypanosomiasis chemotherapy to review the comparative study of 14-day versus 7-day treatment of late stage T. b. gambiense African trypanosomiasis with eflornithine, WHO, Geneva, 14 July 1998. Report on a meeting of the product development team for African trypanosomiasis chemotherapy to review the comparative study of 14 day versus 7 day treatment of late stage T b gambiense African trypanosomiasis with eflornithine, WHO, Geneva, 14 July 1998: 8 pp., 1998

The elimination of human African trypanosomiasis is in sight: Report from the third WHO stakeholders meeting on elimination of gambiense human African trypanosomiasis. Plos Neglected Tropical Diseases 12(12): E0006925, 2018

Studies on Seven-membered Ring Compounds. XXXVI. Synthesis of Azulene Derivatives by Ring Closure of β-Cycloheptatrienyl-substituted Carbonyl Compounds. Chemical & Pharmaceutical Bulletin 19(11): 2215-2221, 1971

Studies on Seven-membered Ring Compounds. XXXV. Ring Closure of -Cycloheptatrienyl-substituted a, b-Unsaturated Carbonyl Compounds to Benzocycloheptene Derivatives. Chemical & Pharmaceutical Bulletin 18(10): 2087-2093, 1970

Transition metal compounds containing substituted imidazole ligands and substituted phenoles as anions. Inorganica Chimica Acta 72: 89-93, 1983

Treatment of human African trypanosomiasis. Bulletin de la Societe de Pathologie Exotique et de Ses Filiales 76(5): 622-627, 1983

Treatment of human African trypanosomiasis. Bulletin of the World Health Organization 78(12): 1474, 2000

The treatment of human African trypanosomiasis. Advances in Parasitology 33: 1-47, 1994

Oxazine Ring-Related Vibrational Modes of Benzoxazine Monomers Using Fully Aromatically Substituted, Deuterated, 15 N Isotope Exchanged, and Oxazine-Ring-Substituted Compounds and Theoretical Calculations. Journal of Physical Chemistry. a 121(33): 6269-6282, 2017

Eflornithine for the treatment of human African trypanosomiasis. Parasitology Research 90 Supp 1: S49-S52, 2003

Some ideas concerning the treatment of African human trypanosomiasis. Bulletin de la Societe Pathologie Exotique et de ses filiales 76(5): 622-627, 1983